期刊
BIOORGANIC CHEMISTRY
卷 67, 期 -, 页码 130-138出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2016.06.004
关键词
7-Substituted coumarins; Anti-inflammatory and analgesic agents; 5-Lipoxygenase inhibitors; Docking
In the present study, 7-subsituted coumarin derivatives were synthesized using various aromatic and heterocyclic amines, and evaluated in vivo for anti-inflammatory and analgesic activity, and for ulcerogenic risk. The most active compounds were evaluated in vitro for 5-lipoxygenase (5-LOX) inhibition. Docking study was performed to predict the binding affinity, and orientation at the active site of the enzyme. In vivo anti-inflammatory and analgesic activity, and in vitro 5-LOX enzyme inhibition study revealed that compound 33 and 35 are the most potent compounds in all the screening methods. In vitro kinetic study of 35 showed mixed or non-competitive type of inhibition with 5-LOX enzyme. Presence of -OCH3 group in 35 and -Cl in 33 at C6-position of benzothiazole ring were found very important substitutions for potent activity. (C) 2016 Published by Elsevier Inc.
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